BIBW2992 (Afatinib) is an irreversible EGFR/HER2 inhibitor with an IC50 of 14 nM for in vitro potency against HER2. In cell-free in vitro kinase assays, BIBW2992 shows potent activity against wild-type and mutant forms of EGFR and HER2, similar to gefitinib in potency for L858R EGFR, but about 100-fold more active against the gefitinib resistant L858R-T790M EGFR double mutant, with an IC50 of 10 nM. BIBW2992 was effective in inhibiting survival of lung cancer cell lines harboring wild-type (H1666) or L858R/T790M (NCI-H1975) EGFR, with IC50s below 100 nM for these isoforms resistant to first-generation inhibitors anda subnanomolar IC50 for the gefitinibsensitive L858R expressedby H3255. Assessed in a standard xenograft model of the epidermoid carcinoma cell line A431. Daily oral treatment with BIBW2992 at 20 mg/kg for 25 days resulted in dramatic tumor regression with a cumulative treated/control tumor volume ratio (T/C ratio) of 2%.

June 21, 2017

prudect name : BIBW2992 (Afatinib) is an irreversible EGFR/HER2 inhibitor with an IC50 of 14 nM for in vitro potency against HER2. In cell-free in vitro kinase assays, BIBW2992 shows potent activity against wild-type and mutant forms of EGFR and HER2, similar to gefitinib in potency for L858R EGFR, but about 100-fold more active against the gefitinib resistant L858R-T790M EGFR double mutant, with an IC50 of 10 nM. BIBW2992 was effective in inhibiting survival of lung cancer cell lines harboring wild-type (H1666) or L858R/T790M (NCI-H1975) EGFR, with IC50s below 100 nM for these isoforms resistant to first-generation inhibitors anda subnanomolar IC50 for the gefitinibsensitive L858R expressedby H3255. Assessed in a standard xenograft model of the epidermoid carcinoma cell line A431. Daily oral treatment with BIBW2992 at 20 mg/kg for 25 days resulted in dramatic tumor regression with a cumulative treated/control tumor volume ratio (T/C ratio) of 2%.
BIBW2992

Synonyms: Tovok, AfatinibCAS NO: 439081-18-2Molecular Formula: C₂₄H₂₅ClFN₅O₃Molecular Weight: 485.94Purity: 99%Solubility: In DMSOStorage: −20°C

Dehydroxymethylepoxyquinomicin References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18505435